Telmisartan

Description	in vitro: In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of 125I-AngII to AT1 receptors in a concentrationdependent manner, with an IC50 of 9.2 ±0.8 nM. The specific binding of [3H]telmisartan to SMC membranes is displaced by unlabeled telmisartan with an IC50 of 7.7± 1.8 nM and by cold AngII with an IC50 of 32.7 5.7 nM. Telmisartan directly prevents angiotensin II (Ang II)-induced endothelial dysfunction (ED) via activating HGF/Met system and/or PPARγ pathway . In cells treated with telmisartan (0.5-2.5 μmol/L) during exposure t non-uniform shear stress, dose-dependent inhibition of monocytic cell adhesion was observed, with about 45% reduction at 1 μmol/L . in vivo: Nine-week-old male db/db mice were fed a 60% high-fat diet, with orally administrated either vehicle (carboxymethyl-cellulose, CMC), 5 mg/kg telmisartan, or 5 mg/kg telmisartan and 1 mg/kg GW9662, a selective irreversible antagonist of PPARγ, for 5 weeks. Effects of telmisartan on Sir
Pathways	GPCR/G Protein
Targets	Angiotensin Receptor

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